DK0572166T3 - New 7beta-substituted-4-aza-5beta-androstan-3-ones as 5beta-reductase inhibitors - Google Patents
New 7beta-substituted-4-aza-5beta-androstan-3-ones as 5beta-reductase inhibitorsInfo
- Publication number
- DK0572166T3 DK0572166T3 DK93303882.0T DK93303882T DK0572166T3 DK 0572166 T3 DK0572166 T3 DK 0572166T3 DK 93303882 T DK93303882 T DK 93303882T DK 0572166 T3 DK0572166 T3 DK 0572166T3
- Authority
- DK
- Denmark
- Prior art keywords
- 5beta
- androstan
- aza
- ones
- substituted
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/40—Unsaturated compounds
- C07C59/76—Unsaturated compounds containing keto groups
- C07C59/80—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings
- C07C59/82—Unsaturated compounds containing keto groups containing rings other than six-membered aromatic rings the keto group being part of a ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/40—Unsaturated compounds
- C07C59/76—Unsaturated compounds containing keto groups
- C07C59/90—Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
- C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
- C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
Abstract
Described are new 7 beta -substituted 4-aza-5 alpha -androstan-3-ones and related compounds as 5 alpha -reductase inhibitors.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88657292A | 1992-05-20 | 1992-05-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
DK0572166T3 true DK0572166T3 (en) | 1997-09-01 |
Family
ID=25389283
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK93303882.0T DK0572166T3 (en) | 1992-05-20 | 1993-05-19 | New 7beta-substituted-4-aza-5beta-androstan-3-ones as 5beta-reductase inhibitors |
Country Status (14)
Country | Link |
---|---|
US (1) | US5710275A (en) |
EP (2) | EP0572166B1 (en) |
JP (1) | JPH06100587A (en) |
CN (1) | CN1087092A (en) |
AT (2) | ATE156838T1 (en) |
CA (1) | CA2096616A1 (en) |
DE (2) | DE69333317T2 (en) |
DK (1) | DK0572166T3 (en) |
ES (2) | ES2106965T3 (en) |
GR (1) | GR3024884T3 (en) |
IL (1) | IL105715A (en) |
MX (1) | MX9302932A (en) |
WO (1) | WO1993023420A1 (en) |
ZA (1) | ZA933497B (en) |
Families Citing this family (39)
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US5237064A (en) * | 1992-05-20 | 1993-08-17 | Merck & Co., Inc. | Process for producing 7β-substituted-aza-5αandrostan-3-ones |
WO1993023051A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors |
JPH07508032A (en) * | 1992-05-20 | 1995-09-07 | メルク エンド カンパニー インコーポレーテッド | Novel Δ-17- and Δ-20 olefinic and saturated 17β-substituted 4-aza-5α-androstan-ones as 5α-reductase inhibitors |
AU672978B2 (en) * | 1992-05-20 | 1996-10-24 | Merck & Co., Inc. | 4-azasteroid 5-alpha-reductase inhibitors |
WO1993023039A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors |
AU675225B2 (en) * | 1992-05-20 | 1997-01-30 | Merck & Co., Inc. | 17-amino substituted 4-azasteroid 5alpha-reductase inhibitors |
WO1993023420A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
US5693810A (en) * | 1992-10-06 | 1997-12-02 | Merck & Co., Inc. | 17 β-carboxanilides of 4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
ATE203162T1 (en) * | 1992-12-18 | 2001-08-15 | Merck & Co Inc | METHOD FOR TREATING CHRONIC PROSTATITIS USING 17-BETA-N-TERTBUTYLCARBAMOYL-4-AZA-5 ALPHA-ANDROST-1-EN-3-ONE |
AU679769B2 (en) * | 1993-06-28 | 1997-07-10 | Merck & Co., Inc. | 4-AZA-pregnane 5alpha-reductase isozyme 1 inhibitors |
US5438061A (en) * | 1993-07-16 | 1995-08-01 | Merck & Co., Inc. | 7-substituted-δ4-6-azasteroid derivatives as 5α-reductase inhibitors |
TW408127B (en) * | 1993-09-17 | 2000-10-11 | Glaxo Inc | Androstenones |
TW369521B (en) * | 1993-09-17 | 1999-09-11 | Smithkline Beecham Corp | Androstenone derivative |
JPH09504553A (en) * | 1993-11-04 | 1997-05-06 | メルク エンド カンパニー インコーポレーテッド | 7-Substituted-4-aza-steroid derivatives as 5α-reductase inhibitors |
US5525608A (en) * | 1994-04-20 | 1996-06-11 | Merck & Co., Inc. | 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors |
GB9415178D0 (en) * | 1994-07-28 | 1994-09-21 | Erba Carlo Spa | 4-azasteroids with side-chain fluoroketones |
US5470976A (en) * | 1994-09-07 | 1995-11-28 | Merck & Co., Inc. | Process for the stereoselective reduction of steroid enelactams |
US5817818A (en) * | 1994-09-16 | 1998-10-06 | Glaxo Wellcome Inc. | Androstenones |
US5541322A (en) * | 1994-10-14 | 1996-07-30 | Glaxo Wellcome Inc. | Synthesis of 6-azaandrostenones |
US5656613A (en) * | 1995-01-04 | 1997-08-12 | Merck & Co., Inc. | Treatment of hyperandrogenic conditions |
US5763361A (en) * | 1995-10-23 | 1998-06-09 | Merck & Co., Inc. | 17-alkyl-7-substituted-4-aza steroid derivatives as 5-α-reductase inhibitors |
EP0862556B1 (en) * | 1995-10-23 | 2001-09-05 | Merck & Co., Inc. | 17-alkyl-7-substituted-4-aza steroid derivatives |
US6365597B1 (en) | 1996-02-14 | 2002-04-02 | Aventis Pharmaceuticals Inc. | 4-aza steroids |
US5872126A (en) * | 1996-09-06 | 1999-02-16 | Merck & Co., Inc. | Methods and compositions for treating preterm labor |
WO1998050419A2 (en) * | 1997-05-07 | 1998-11-12 | Novopharm Limited | 4-aza-steroids as inhibitors of testosterone-5-alpha-reductase |
US5998427A (en) * | 1998-05-14 | 1999-12-07 | Glaxo Wellcome Inc. | Androstenones |
WO2003059293A2 (en) * | 2002-01-15 | 2003-07-24 | Merck & Co., Inc. | 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators |
CA2524409C (en) * | 2003-05-07 | 2011-12-20 | Merck & Co., Inc. | Androgen receptor modulators and methods of use thereof |
EP1641464A4 (en) * | 2003-06-30 | 2008-05-14 | Merck & Co Inc | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
JP2007521297A (en) * | 2003-06-30 | 2007-08-02 | メルク エンド カムパニー インコーポレーテッド | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
US7482357B2 (en) | 2003-06-30 | 2009-01-27 | Merck & Co., Inc. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
AU2004256075B2 (en) * | 2003-06-30 | 2008-12-04 | Merck Sharp & Dohme Corp. | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
AU2004272004B2 (en) | 2003-09-10 | 2009-01-22 | Merck Sharp & Dohme Corp. | 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
CA2537660A1 (en) * | 2003-09-10 | 2005-03-24 | Merck & Co., Inc. | 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators |
CA2562132A1 (en) * | 2004-04-08 | 2005-10-27 | Merck & Co., Inc. | 17 beta-acetamide-4-azasteroids as androgen receptor modulators |
CN100355772C (en) * | 2005-12-28 | 2007-12-19 | 天津大学 | Steroid compound with 5-alpha reductase active and preparation process thereof |
WO2011131543A1 (en) * | 2010-04-20 | 2011-10-27 | Syngenta Participations Ag | Process for the preparation of pyrazole carboxylic acid amides |
CN111175410A (en) * | 2020-02-12 | 2020-05-19 | 武汉大学 | Application of N-methyl phenethylamine and isotope reagent thereof in detection of carboxyl compound |
CN117858887A (en) * | 2021-06-16 | 2024-04-09 | 拉瓦勒大学 | Novel inhibitors of 17 beta-HSD 7 and uses thereof |
Family Cites Families (26)
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AU527030B2 (en) * | 1978-04-13 | 1983-02-10 | Merck & Co., Inc. | 4-aza-17-substituted-5a-androstan-3-ones |
US4377584A (en) * | 1978-04-13 | 1983-03-22 | Merck & Co., Inc. | 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors |
US4220775A (en) * | 1979-03-15 | 1980-09-02 | Merck & Co., Inc. | Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors |
EP0314199B1 (en) * | 1984-02-27 | 1991-09-18 | Merck & Co. Inc. | 17 beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors |
US4760071A (en) * | 1984-02-27 | 1988-07-26 | Merck & Co., Inc. | 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors |
US5049562A (en) * | 1984-02-27 | 1991-09-17 | Merck & Co., Inc. | 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors |
NZ211145A (en) * | 1984-02-27 | 1988-10-28 | Merck & Co Inc | 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions |
US5138063A (en) * | 1984-02-27 | 1992-08-11 | Merck & Co., Inc. | 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones |
US4859681A (en) * | 1984-02-27 | 1989-08-22 | Merck & Co., Inc. | 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors |
US4888336A (en) * | 1987-01-28 | 1989-12-19 | Smithkline Beckman Corporation | Steroid 5-alpha-reductase inhibitors |
US5026882A (en) * | 1988-12-23 | 1991-06-25 | Smithkline Beecham Corporation | Phosphinic acid substituted steroids as inhibitors of steroid 5α-reductase |
US5032586A (en) * | 1989-08-24 | 1991-07-16 | Smithkline Beecham Corporation | 7-keto or hydroxy 3,5-diene steroids as inhibitors of steroid 5-alpha reductase |
US5300294A (en) * | 1990-06-27 | 1994-04-05 | Smithkline Beecham Corporation | Method of treating prostatic adenocarcinoma |
IE76452B1 (en) * | 1990-10-29 | 1997-10-22 | Sankyo Co | Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use |
CA2084799C (en) * | 1991-12-17 | 2003-01-28 | Glenn J. Gormley | Method of prevention of prostatic carcinoma with 17 beta-n-monosubstituted-carbamoyl-4-aza-5 alpha-androst-1 -en-3-ones |
ATE165368T1 (en) * | 1991-12-20 | 1998-05-15 | Glaxo Wellcome Inc | INHIBITORS OF TESTOSTERONE-5-ALPHA REDUCTASE. |
US5215894A (en) * | 1992-02-25 | 1993-06-01 | Merck & Co., Inc. | Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors |
WO1993023051A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | New 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5a-reductase inhibitors |
CZ283894A3 (en) * | 1992-05-20 | 1995-09-13 | Merck & Co Inc | 7beta-substituted 4-aza-5alpha-cholestanones, their use for the preparation of pharmaceutical preparations and pharmaceutical compositions containing thereof |
WO1993023420A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS |
WO1993023040A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | 17-ethers and thioethers of 4-aza-steroids |
JPH07508032A (en) * | 1992-05-20 | 1995-09-07 | メルク エンド カンパニー インコーポレーテッド | Novel Δ-17- and Δ-20 olefinic and saturated 17β-substituted 4-aza-5α-androstan-ones as 5α-reductase inhibitors |
US5237064A (en) * | 1992-05-20 | 1993-08-17 | Merck & Co., Inc. | Process for producing 7β-substituted-aza-5αandrostan-3-ones |
UA35589C2 (en) * | 1992-05-21 | 2001-04-16 | Андорешерш Інк. | INHIBITORS OF TESTOSTERONE 5-<font face="Symbol">a</font>-REDUCTASE activity, pharmaceutical composition and a method for inhibiting activity of testosterone 5-<font face="Symbol">a</font>-REDUCTASE |
US5278159A (en) * | 1992-10-06 | 1994-01-11 | Merck & Co., Inc. | Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors |
US5543417A (en) * | 1994-10-21 | 1996-08-06 | Merck & Co., Inc. | Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents |
-
1993
- 1993-05-14 WO PCT/US1993/004643 patent/WO1993023420A1/en active Application Filing
- 1993-05-14 US US08/341,602 patent/US5710275A/en not_active Expired - Fee Related
- 1993-05-17 IL IL105715A patent/IL105715A/en not_active IP Right Cessation
- 1993-05-19 EP EP93303882A patent/EP0572166B1/en not_active Expired - Lifetime
- 1993-05-19 AT AT93303882T patent/ATE156838T1/en not_active IP Right Cessation
- 1993-05-19 DK DK93303882.0T patent/DK0572166T3/en active
- 1993-05-19 ES ES93303882T patent/ES2106965T3/en not_active Expired - Lifetime
- 1993-05-19 ZA ZA933497A patent/ZA933497B/en unknown
- 1993-05-19 DE DE69333317T patent/DE69333317T2/en not_active Expired - Fee Related
- 1993-05-19 AT AT96202933T patent/ATE255125T1/en not_active IP Right Cessation
- 1993-05-19 ES ES96202933T patent/ES2210336T3/en not_active Expired - Lifetime
- 1993-05-19 CA CA002096616A patent/CA2096616A1/en not_active Abandoned
- 1993-05-19 MX MX9302932A patent/MX9302932A/en not_active IP Right Cessation
- 1993-05-19 DE DE69313018T patent/DE69313018T2/en not_active Expired - Fee Related
- 1993-05-19 EP EP96202933A patent/EP0778284B1/en not_active Expired - Lifetime
- 1993-05-19 CN CN93107704A patent/CN1087092A/en active Pending
- 1993-05-20 JP JP5154097A patent/JPH06100587A/en active Pending
-
1997
- 1997-09-30 GR GR970402529T patent/GR3024884T3/en unknown
Also Published As
Publication number | Publication date |
---|---|
WO1993023420A1 (en) | 1993-11-25 |
DE69313018T2 (en) | 1998-02-19 |
US5710275A (en) | 1998-01-20 |
AU3869893A (en) | 1993-11-25 |
CA2096616A1 (en) | 1993-11-21 |
AU662224B2 (en) | 1995-08-24 |
EP0572166B1 (en) | 1997-08-13 |
JPH06100587A (en) | 1994-04-12 |
MX9302932A (en) | 1995-01-31 |
DE69333317D1 (en) | 2004-01-08 |
IL105715A0 (en) | 1993-09-22 |
ATE255125T1 (en) | 2003-12-15 |
GR3024884T3 (en) | 1998-01-30 |
CN1087092A (en) | 1994-05-25 |
EP0778284B1 (en) | 2003-11-26 |
DE69313018D1 (en) | 1997-09-18 |
EP0778284A2 (en) | 1997-06-11 |
ES2210336T3 (en) | 2004-07-01 |
IL105715A (en) | 1997-07-13 |
EP0778284A3 (en) | 1997-08-13 |
DE69333317T2 (en) | 2004-08-19 |
ES2106965T3 (en) | 1997-11-16 |
EP0572166A1 (en) | 1993-12-01 |
ZA933497B (en) | 1993-12-14 |
ATE156838T1 (en) | 1997-08-15 |
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